2. Cell Cycle/DNA Damage Apoptosis
  3. Antifolate Apoptosis Caspase Bcl-2 Family
  4. Lometrexol disodium

Lometrexol disodium  (Synonyms: DDATHF disodium)

目录号: HY-14521A 纯度: ≥98.0%
COA 产品使用指南

摩尔计算器

Lometrexol (DDATHF) disodium 是一种抗嘌呤类抗叶酸 (antifolate) 药，可抑制甘氨酰胺核糖核苷酸甲酰基转移酶 (GARFT) 的活性，但不会引起可检测水平的 DNA 链断裂。Lometrexol disodium 可以进一步抑制嘌呤从头合成，导致异常的细胞增殖，凋亡 (apoptosis) 和细胞周期停滞。Lometrexol disodium 具有抗癌活性。Lometrexol disodium 还是一种有效的人丝氨酸羟甲基转移酶 1/2 (hSHMT1/2) 抑制剂。

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Lometrexol disodium Chemical Structure

Lometrexol disodium Chemical Structure

CAS No. : 120408-07-3

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1 mg ￥2300
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Other Forms of Lometrexol disodium:

Lometrexol disodium 相关抗体

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MCE 顾客使用本产品发表的 1 篇科研文献

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Lometrexol (DDATHF) disodium, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol disodium can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol disodium has anticancer activity. Lometrexol disodium also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor[1][2][3].

体外研究
(In Vitro)

Lometrexol (DDATHF) disodium binds tightly to GART, resulting in a rapid and prolonged depletion of intracellular purine ribonucleotides[3].
Lometrexol (1-30 μM; 2-10 hours) disodium induces rapid and complete growth inhibition in L1210 cells[3].
Lometrexol (1 μM; 2-24 hours) disodium induces cell cycle arrest in murine leukemia L1210 cells[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Lometrexol disodium 相关抗体:

Cell Viability Assay[3]

Cell Line: Mouse leukemia L1210 cells
Concentration: 1, 30 μM
Incubation Time: 2, 4, 6, 8, 10 hours
Result: Induced rapid and complete growth inhibition.

Cell Cycle Analysis[3]

Cell Line: L1210 cells
Concentration: 1 μM
Incubation Time: 2, 4, 8, 12, 24 hours
Result: Caused a rapid loss of the G2/M phase population of cells and an early S phase accumulation of cells by 8 hours. By 24 h, the S phase population appeared to be slowly shifting to higher DNA content, and hence, from mid-to-late S phase.
体内研究
(In Vivo)

Lometrexol (DDATHF; i.p.; 15-60 mg/kg; on gestation day 7.5) disodium induces neural tube defects (NTDs) by disturbing purine metabolism and increases the rate of embryonic resorption and growth retardation in a dose-dependent manner[1].
Lometrexol (i.p.; 40 mg/kg; on gestation day 7.5) disodium decreases glycinamide ribonucleotide formyl transferase (GARFT) activity and Changes of ATP, GTP, dATP and dGTP levels[1].
Lometrexol (i.p.; 40 mg/kg; on gestation day 7.5) disodium induces abnormal proliferation and apoptosis exist in neural tube defects (NTDs)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice (7-8 week, 18-20 g)[1]
Dosage: 15, 30, 35, 40, 45 and 60 mg/kg
Administration: Intraperitoneal injection; on gestation day 7.5
Result: Increased the rate of embryonic resorption and growth retardation in a dose-dependent manner.
Animal Model: C57BL/6 mice (7-8 week, 18-20 g)[1]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection; on gestation day 7.5, for 0, 6, 24, 48 and 96 hours
Result: Inhibited glycinamide ribonucleotide formyl transferase (GARFT) activity and GARFT activity was maximally inhibited after at 6 hours.
Decreased the levels of ATP, GTP, dATP, and dGTP of NTDs embryonic brain tissue significantly at 6 hours.
Animal Model: C57BL/6 mice (7-8 week, 18-20 g)[1]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection; on gestation day 7.5, for 4 days
Result: Decreased the expression of proliferation-related genes (Pcna, Foxg1 and Ptch1) and increased the expression of apoptosis-related genes (Bax, Casp8 and Casp9) in NTD groups.
Clinical Trial
分子量

487.42

Formula

C21H23N5Na2O6
CAS 号
性状

固体

颜色

White to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验： 

H2O 中的溶解度 : 100 mg/mL (205.16 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0516 mL 10.2581 mL 20.5162 mL
5 mM 0.4103 mL 2.0516 mL 4.1032 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: ≥98.0%

COA (285 KB)

产品使用指南 (1538 KB)
参考文献

Lometrexol disodium 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 2.0516 mL 10.2581 mL 20.5162 mL 51.2905 mL
5 mM 0.4103 mL 2.0516 mL 4.1032 mL 10.2581 mL
10 mM 0.2052 mL 1.0258 mL 2.0516 mL 5.1290 mL
15 mM 0.1368 mL 0.6839 mL 1.3677 mL 3.4194 mL
20 mM 0.1026 mL 0.5129 mL 1.0258 mL 2.5645 mL
25 mM 0.0821 mL 0.4103 mL 0.8206 mL 2.0516 mL
30 mM 0.0684 mL 0.3419 mL 0.6839 mL 1.7097 mL
40 mM 0.0513 mL 0.2565 mL 0.5129 mL 1.2823 mL
50 mM 0.0410 mL 0.2052 mL 0.4103 mL 1.0258 mL
60 mM 0.0342 mL 0.1710 mL 0.3419 mL 0.8548 mL
80 mM 0.0256 mL 0.1282 mL 0.2565 mL 0.6411 mL
100 mM 0.0205 mL 0.1026 mL 0.2052 mL 0.5129 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lometrexol disodium120408-07-3DDATHF disodiumAntifolateApoptosisCaspaseBcl-2 FamilyantipurineantifolateGARFTnovopurinesynthesiscellproliferationapoptosiscyclearrestleukemiaL1210Inhibitorinhibitorinhibit

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